Glycolipids as host resistance stimulators.
6-(5-Cholesten-3 beta-yloxy)hexyl 1-thio-beta-D-mannopyranoside (L-644,257) enhances natural host resistance in cyclophosphamide-treated mice against Pseudomonas aeruginosa in a dose-dependent manner. It is active sc, im, and ip but not orally. L-644,257 is substantially more protective against P. aeruginosa than its alpha anomer. The beta-L-fucose glycolipid is more effective when given im and ip than sc. The lactose and beta-D-glucose glycolipids were only marginally effective to nonprotective. The 17 beta-steroidal side chain of L-644,257 can be modified without substantial loss of protective activity.
Ponpipom
M M
MM
Merck Sharp & Dohme Research Laboratories, Rahway, New Jersey 07065.
Hagmann
W K
WK
O'Grady
L A
LA
Jackson
J J
JJ
Wood
D D
DD
Zweerink
H J
HJ
D000276:Adjuvants, Immunologic; D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D002784:Cholesterol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D005260:Female; D006017:Glycolipids / Q000009:adverse effects / Q000494:pharmacology*; D007167:Immunotherapy; D051379:Mice; D009894:Opportunistic Infections / Q000628:therapy*; D011552:Pseudomonas Infections / Q000628:therapy; D013329:Structure-Activity Relationship
D000276:Adjuvants, Immunologic; D006017:Glycolipids; C030513:L 644257; D002784:Cholesterol